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Assay Detail

CHEMBL863544

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
May JA, Dantanarayana AP, Zinke PW, McLaughlin MA, Sharif NA.
J Med Chem (2006) 49 : 318 -328
PubMed 16392816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.28 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197653 1 9.00
CHEMBL373245 1 8.92
CHEMBL199775 1 8.82
CHEMBL371300 1 8.52
CHEMBL200104 1 8.44
CHEMBL134519 1 8.40
CHEMBL201132 1 8.32
CHEMBL275854 1 8.15
CHEMBL39 SEROTONIN 3.0 1 8.08
CHEMBL31115 1 8.08
CHEMBL199385 1 8.02
CHEMBL437314 1 7.47
CHEMBL7257 MEBUFOTENIN 2.0 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197653 Ki = 1.0 nM 9.00
CHEMBL373245 Ki = 1.2 nM 8.92
CHEMBL199775 Ki = 1.5 nM 8.82
CHEMBL371300 Ki = 3.0 nM 8.52
CHEMBL200104 Ki = 3.6 nM 8.44
CHEMBL134519 Ki = 4.0 nM 8.40
CHEMBL201132 Ki = 4.8 nM 8.32
CHEMBL275854 Ki = 7.0 nM 8.15
CHEMBL39 SEROTONIN Ki = 8.3 nM 8.08
CHEMBL31115 Ki = 8.3 nM 8.08
CHEMBL199385 Ki = 9.6 nM 8.02
CHEMBL437314 Ki = 34.0 nM 7.47
CHEMBL7257 MEBUFOTENIN Ki = 42.0 nM 7.38